Name: Darifenacin HBr
Brand: Selleck Chemicals
SKU: S3144
Availability: InStock
Rating: 5 (3 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Adrenergic Receptor 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other AChR Inhibitors	PNU-120596 Benzethonium Chloride Arecoline HBr Lycorine Otilonium Bromide Hyoscyamine (-)-Huperzine A (HupA) Nitenpyram Cytisine Palmatine

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
HEK cells	Function assay			Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay, EC50=0.00082 μM
H292 cells	Function assay			Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins, EC50=0.01585 μM
HEK293 cells	Function assay			Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting, EC50=0.0007943 μM
CHO-K1 cells	Function assay			Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50=1.58489 μM
PC3	Proliferation assay	10 μM and 20 μM		blockade of CHRM3 by darifenacin could effectively reduce cell proliferation
22Rv1	Proliferation assay	10 μM and 20 μM		blockade of CHRM3 by darifenacin could effectively reduce cell proliferation
H1299	Proliferation assay	0.3–100 µM	72 h	significantly inhibited H1299 cell proliferation in a concentration-dependent manner
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 117 mg/mL (230.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.710mg/ml (1.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	507.46	Formula	C₂₈H₃₀N₂O₂.HBr	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	133099-07-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	UK-88525			Smiles	C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5.Br

Mechanism of Action

Targets/IC₅₀/Ki	M3 mAChR 8.9(pKi)
In vitro	Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 µM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6.
In vivo	Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBC_AMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers. Darifenacin (7.5 mg and 15 mg, daily) reduces the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also shows significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, severity of urgency and number of incontinence episodes leading to a change in clothing or pads in patients with overactive bladder (OAB).
References	[1] https://pubmed.ncbi.nlm.nih.gov/9113359/ [2] https://pubmed.ncbi.nlm.nih.gov/21826715/ [3] https://pubmed.ncbi.nlm.nih.gov/17360104/ [4] https://pubmed.ncbi.nlm.nih.gov/15041104/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00703703	Completed	Healthy	Novartis\|Procter and Gamble	May 2008	Phase 1
NCT00921245	Completed	Overactive Bladder	Bayer	June 2007	--
NCT00413790	Completed	Healthy	Novartis\|Procter and Gamble	November 2006	Phase 4
NCT00413426	Completed	Healthy	Novartis\|Procter and Gamble	June 2006	Phase 1
NCT00366002	Completed	Overactive Bladder (OAB)	Novartis\|Procter and Gamble	June 2006	Phase 4

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Handling Instructions

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Darifenacin HBr AChR antagonist

Chemical Structure

Molecular Weight: 507.46